Oral controlled release dosage form
First Claim
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1. A controlled release methylphenidate tablet consisting of:
- (A) an immediate release methylphenidate coating consisting of;
(a) 30-60 weight percent based upon the total weight of the immediate release coating of methylphenidate or a pharmaceutically acceptable salt or isomer thereof;
(b) 40-70 weight percent based upon the total weight of the immediate release coating of a binder; and
(c) 0.005-5 weight percent based upon the total weight of the immediate release coating of an organic acid;
(B) a controlled release methylphenidate core tablet consisting of;
(a) a compressed mixture consisting of;
(i) 5-40 weight percent based upon the total weight of the compressed mixture of methylphenidate or a pharmaceutically acceptable salt or isomer thereof;
(ii) 3-40 weight percent based upon the total weight of the compressed mixture of a hydrogel polymer;
(iii) 25-90 weight percent based upon the total weight of the compressed mixture of a diluent; and
(iv) optionally a lubricant; and
(b) an enteric coating surrounding the core tablet consisting of;
(i) 10-70 weight percent based upon the total weight of the enteric coating of a methacrylic acid copolymer;
(ii) 1-5 weight percent based upon the total weight of the enteric coating of a plasticizer;
(iii) an anti-sticking agent; and
(iv) optionally a surfactant; and
(C) optionally an aesthetic coating;
wherein the controlled release methylphenidate tablet exhibits the following dissolution profile when tested in a United States Pharmacopeia type 2 (paddle) apparatus at 50 rpms in 900 ml of phosphate buffer with a pH of 7.5 and at 37°
C.;
1-35% of the methylphenidate is released after 1 hour;
5-40% of the methylphenidate is released after 2 hours; and
not less than 70% is release after 10 hours; and
when administered to humans exhibits a plasma peak for the immediate release layer (Tmax1) between 1 and 5 hours, a plasma peak for the controlled release core (Tmax2) between 4 and 12 hours, and a plasma trough (Tmin) between 2 and 7 hours in between the two peak plasma levels; and
wherein the immediate release methylphenidate coating (A) is applied to the enteric coating surrounding the core tablet.
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Abstract
A dosage form that provides a controlled release solid dosage form for the oral administration of a central nervous system stimulant, preferably methylphenidate hydrochloride.
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Citations
13 Claims
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1. A controlled release methylphenidate tablet consisting of:
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(A) an immediate release methylphenidate coating consisting of; (a) 30-60 weight percent based upon the total weight of the immediate release coating of methylphenidate or a pharmaceutically acceptable salt or isomer thereof; (b) 40-70 weight percent based upon the total weight of the immediate release coating of a binder; and (c) 0.005-5 weight percent based upon the total weight of the immediate release coating of an organic acid; (B) a controlled release methylphenidate core tablet consisting of; (a) a compressed mixture consisting of; (i) 5-40 weight percent based upon the total weight of the compressed mixture of methylphenidate or a pharmaceutically acceptable salt or isomer thereof; (ii) 3-40 weight percent based upon the total weight of the compressed mixture of a hydrogel polymer; (iii) 25-90 weight percent based upon the total weight of the compressed mixture of a diluent; and (iv) optionally a lubricant; and (b) an enteric coating surrounding the core tablet consisting of; (i) 10-70 weight percent based upon the total weight of the enteric coating of a methacrylic acid copolymer; (ii) 1-5 weight percent based upon the total weight of the enteric coating of a plasticizer; (iii) an anti-sticking agent; and (iv) optionally a surfactant; and (C) optionally an aesthetic coating; wherein the controlled release methylphenidate tablet exhibits the following dissolution profile when tested in a United States Pharmacopeia type 2 (paddle) apparatus at 50 rpms in 900 ml of phosphate buffer with a pH of 7.5 and at 37°
C.;1-35% of the methylphenidate is released after 1 hour; 5-40% of the methylphenidate is released after 2 hours; and not less than 70% is release after 10 hours; and when administered to humans exhibits a plasma peak for the immediate release layer (Tmax1) between 1 and 5 hours, a plasma peak for the controlled release core (Tmax2) between 4 and 12 hours, and a plasma trough (Tmin) between 2 and 7 hours in between the two peak plasma levels; and
wherein the immediate release methylphenidate coating (A) is applied to the enteric coating surrounding the core tablet. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13)
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Specification